Adenosine
(Synonyms: 腺苷; Adenine riboside; D-Adenosine) 目录号 : GC14106
Adenosine是一种内源性神经调节物质，包含腺嘌呤，通过β-N9-糖苷键与核糖分子（呋喃核糖）部分连接。
Cas No.:58-61-7
Sample solution is provided at 25 µL, 10mM.
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Adenosine is an endogenous neuroregulatory substance, containing adenine, which is linked to the ribose molecule (furanose) through a β-N9-glycosidic bond [1]. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and hematopoietic regulation. Adenosine can be used to treat supraventricular tachycardia [2].
In vitro, different concentrations of Adenosine (1.0-4.0mM; 12, 24 and 48 hours) inhibited the survival rate of HepG2 cells in a time- and dose-dependent manner, significantly increased the mRNA and protein levels of GRP78/BiP, PERK, ATF4, CHOP, caspase-3, and cytochrome c, reduced mitochondrial membrane potential, and activated endoplasmic reticulum stress [3]. Adenosine (0.5-4.0mM; 36 hours) significantly increased the expression of caspase-3 in EC109 cells in a dose-dependent manner, induce cell apoptosis and NF-κB activation [4].
In vivo, Adenosine (1-10mg/kg/day; i.p.) was administered as a single dose to mice in the forced swimming test (FST) and tail suspension test (TST), significantly shortening the immobility time in FST and producing a similar antidepressant-like effect in TST [5]. Adenosine (5mg/kg/day; i.p.; six times, at one-hour intervals) treatment in mice increased the expression level of the inflammatory reactive astrocyte marker (Lcn 2), and simultaneously enhanced the expression of several other pro-inflammatory cytokine/cytokine chemotactic factor genes, such as Ccl 2, Cxcl 1, Ilia and Tnf [6].
References:
[1] Fredholm B B, Chen J F, Cunha R A, et al. Adenosine and brain function[J]. Int Rev Neurobiol, 2005, 63(1): 191-270.
[2] Borea PA, Gessi S, Merighi S, et al. Pharmacology of Adenosine Receptors: The State of the Art. Physiol Rev. 2018 Jul 1;98(3):1591-1625.
[3] Zhou XT, Pu ZJ, Liu LX,,et al.. Inhibition of autophagy enhances adenosine‑induced apoptosis in human hepatoblastoma HepG2 cells. Oncol Rep. 2019 Feb;41(2):829-838.
[4] Wu L F, Wei B L, Guo Y T, et al. Apoptosis induced by adenosine involves endoplasmic reticulum stress in EC109 cells[J]. International journal of molecular medicine, 2012, 30(4): 797-804.
[5] Kaster MP, Rosa AO, Rosso MM, et al. Adenosine administration produces an antidepressant-like effect in mice: evidence for the involvement of A1 and A2A receptors. Neurosci Lett. 2004;355(1-2):21-24.
[6] Guo Q, Gobbo D, Zhao N, et al. Adenosine triggers early astrocyte reactivity that provokes microglial activation and drives the pathogenesis of sepsis-associated encephalopathy[J]. bioRxiv, 2023: 2023.10. 30.563169.
Adenosine是一种内源性神经调节物质，包含腺嘌呤，通过β-N9-糖苷键与核糖分子（呋喃核糖）部分连接 [1]。Adenosine几乎影响细胞生理学的所有方面，包括神经元活动、血管功能、血小板聚集和血细胞调节。Adenosine能够用于治疗室上性心动过速 [2]。
在体外，不同浓度的Adenosine（1.0-4.0mM; 12、24和48h）能够以时间和剂量依赖性方式抑制HepG 2细胞的存活率，显著升高GRP 78/BiP、PERK、ATF 4、CHOP、caspase-3、细胞色素c的mRNA和蛋白水平，降低线粒体膜电位，激活内质网应激 [3]。Adenosine（0.5-4.0mM; 36h）能够以剂量依赖性方式显著增加EC 109细胞caspase-3的表达，诱导细胞凋亡和NF-κB活化 [4]。
在体内，Adenosine（1-10mg/kg/day；i.p.）单次给药治疗强迫游泳试验（FST）和悬尾试验（TST）小鼠，显著缩短了FST中的不动时间，在TST中产生类似抗抑郁药的作用 [5]。Adenosine（5mg/kg/day；i.p.；六次，每次间隔一小时）治疗小鼠，上调了炎性反应性星形胶质细胞的标志物（Lcn 2）的表达水平，同时增加了几种其他促炎细胞因子/趋化因子基因，如Ccl 2、Cxcl 1、Illa和Tnf的表达 [6]。
| Cell experiment [1]: | |
Cell lines | Human hepatoblastoma HepG2 cell line |
Preparation Method | HepG2 cells were seeded in a 96-well plate (5×103 cells/well) in a humidified atmosphere with 5% CO2 at 37°C and treated with Adenosine alone (0, 1.0, 2.0, 3.0 and 4.0mM) for 12, 24 and 48 h; or 10µM LY 294002 alone or 2.0mM Adenosine in combination with 10µM LY 294002 for 12, 24, 36 and 48h. Subsequently, 10µl MTT (5mg/ml) was added to each well and cells were incubated for an additional 4h. Following removal of the supernatant, DMSO (100µl/well) was added to dissolve the blue formazan crystals converted from MTT by HepG2 cells. Cell viability was assessed using a microplate reader at an optical density of 560nm (Wellscan K3; KHB Labsystems, Helsinki, Finland). The experiment was repeated three times. |
Reaction Conditions | 0, 1, 2, 3, and 4mM; 12, 24 and 48h |
Applications | Adenosine inhibited cell viability in a time- and dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Swiss mice |
Preparation Method | Swiss mice of either sex, weighing 30–40g were maintained at constant room temperature (22–27°C) with free access to water and food, under a 12:12h light:dark cycle (lights on at 07:00h). All manipulations were carried out between 09:00 and 17:00h, with each animal used only once. Adenosine and caffeine were dissolved in saline. The drugs were administered by intraperitoneal (i.p.) route in a volume of 10mg/kg body weight. Adenosine or vehicle was administered i.p. 30min before the FST, TST or open-field test. Alternatively, in order to assess its central effect, Adenosine was administered by intracerebroventricular (i.c.v.) route 15min before the FST or open-field test. I.c.v. injections were given under light ether anesthesia. Saline or Adenosine was injected in a volume of 5μl, given over 30s, and the cannula remained in place for a further 30s. |
Dosage form | 1-10mg/kg; i.p. |
Applications | Adenosine administered both by i.p. and i.c.v. route significantly decreased the duration of immobility in the FST. |
References: | |
| Cas No. | 58-61-7 | SDF | |
| 别名 | 腺苷; Adenine riboside; D-Adenosine | ||
| 化学名 | (2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol | ||
| Canonical SMILES | C1=NC2=C(C(=N1)N)N=CN2C3C(C(C(O3)CO)O)O | ||
| 分子式 | C10H13N5O4 | 分子量 | 267.24 |
| 溶解度 | ≥ 12.75mg/mL in DMSO with gentle warming | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.742 mL | 18.7098 mL | 37.4195 mL |
| 5 mM | 0.7484 mL | 3.742 mL | 7.4839 mL |
| 10 mM | 0.3742 mL | 1.871 mL | 3.742 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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